Redox-Responsive, Core-Cross-Linked Micelles Capable of On-Demand, Concurrent Drug Release and Structure Disassembly

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• 作者：Hua Wang ; Li Tang ; Chunlai Tu ; Ziyuan Song ; Qian Yin ; Lichen Yin ; Zhonghai Zhang ; Jianjun Cheng
• 刊名：Biomacromolecules
• 出版年：2013
• 出版时间：October 14, 2013
• 年：2013
• 卷：14
• 期：10
• 页码：3706-3712
• 全文大小：474K
• 年卷期：v.14,no.10(October 14, 2013)
• ISSN：1526-4602

文摘

We developed camptothecin (CPT)-conjugated, core-cross-linked (CCL) micelles that are subject to redox-responsive cleavage of the built-in disulfide bonds, resulting in disruption of the micellar structure and rapid release of CPT. CCL micelles were prepared via coprecipitation of disulfide-containing CPT-poly(tyrosine(alkynyl)-OCA) conjugate and monomethoxy poly(ethylene glycol)-b-poly(tyrosine(alkynyl)-OCA), followed by cross-linking of the micellar core via azide鈥揳lkyne click chemistry. CCL micelles exhibited excellent stability under physiological conditions, while they underwent rapid dissociation in reduction circumstance, resulting in burst release of CPT. These redox-responsive CCL micelles showed enhanced cytotoxicity against human breast cancer cells in vitro.